JP2016512213A5 - - Google Patents
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- JP2016512213A5 JP2016512213A5 JP2015562166A JP2015562166A JP2016512213A5 JP 2016512213 A5 JP2016512213 A5 JP 2016512213A5 JP 2015562166 A JP2015562166 A JP 2015562166A JP 2015562166 A JP2015562166 A JP 2015562166A JP 2016512213 A5 JP2016512213 A5 JP 2016512213A5
- Authority
- JP
- Japan
- Prior art keywords
- less
- peptide
- peg
- receptor
- glp
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 102000025873 GPCR, family 2, glucagon receptor Human genes 0.000 claims 9
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 claims 9
- 239000004472 Lysine Substances 0.000 claims 7
- 230000000694 effects Effects 0.000 claims 7
- 108010063919 GPCR, family 2, glucagon receptor Proteins 0.000 claims 6
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 claims 6
- DTHNMHAUYICORS-KTKZVXAJSA-N 107444-51-9 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 5
- 150000001413 amino acids Chemical group 0.000 claims 5
- 102000004965 antibodies Human genes 0.000 claims 5
- 108090001123 antibodies Proteins 0.000 claims 5
- 230000027455 binding Effects 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 101710042131 GCG Proteins 0.000 claims 4
- 102100005236 ZGLP1 Human genes 0.000 claims 4
- 101700078733 ZGLP1 Proteins 0.000 claims 4
- 101700071595 GRZ1 Proteins 0.000 claims 3
- 108060003199 Glucagon Proteins 0.000 claims 3
- 229960004666 Glucagon Drugs 0.000 claims 3
- MASNOZXLGMXCHN-ZLPAWPGGSA-N Glucagonum Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 claims 3
- 102000008100 Human Serum Albumin Human genes 0.000 claims 3
- 108091006822 Human Serum Albumin Proteins 0.000 claims 3
- 239000000556 agonist Substances 0.000 claims 3
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 claims 3
- FUOOLUPWFVMBKG-UHFFFAOYSA-N α-aminoisobutanoic acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 3
- 102100001249 ALB Human genes 0.000 claims 2
- 101710027066 ALB Proteins 0.000 claims 2
- 229940050528 albumin Drugs 0.000 claims 2
- 238000004166 bioassay Methods 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 101500013968 human Glucagon Proteins 0.000 claims 2
- 101500013969 human Glucagon-like peptide 1 Proteins 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
- 229920001184 polypeptide Polymers 0.000 claims 2
- GUOSQNAUYHMCRU-UHFFFAOYSA-N 11-Aminoundecanoic acid Chemical group NCCCCCCCCCCC(O)=O GUOSQNAUYHMCRU-UHFFFAOYSA-N 0.000 claims 1
- SLXKOJJOQWFEFD-UHFFFAOYSA-N Aminocaproic acid Chemical group NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims 1
- 229940019746 Antifibrinolytic amino acids Drugs 0.000 claims 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 claims 1
- 101700077246 EHMT1 Proteins 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 102100014838 FCGRT Human genes 0.000 claims 1
- 101710003435 FCGRT Proteins 0.000 claims 1
- 101710004768 GER5 Proteins 0.000 claims 1
- 101710004110 GLP Proteins 0.000 claims 1
- 101700022962 HSP12 Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 101710042151 Os01g0681900 Proteins 0.000 claims 1
- 101710039481 Os03g0179100 Proteins 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 102100014963 PEG3 Human genes 0.000 claims 1
- 101700039549 PEG3 Proteins 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 210000002966 Serum Anatomy 0.000 claims 1
- 208000001072 Type 2 Diabetes Mellitus Diseases 0.000 claims 1
- 229960002684 aminocaproic acid Drugs 0.000 claims 1
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 1
- 229960002685 biotin Drugs 0.000 claims 1
- 235000020958 biotin Nutrition 0.000 claims 1
- 239000011616 biotin Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229920000592 inorganic polymer Polymers 0.000 claims 1
- 101500013990 mouse Glucagon Proteins 0.000 claims 1
- 101500013991 mouse Glucagon-like peptide 1 Proteins 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229920000620 organic polymer Polymers 0.000 claims 1
- 235000020825 overweight Nutrition 0.000 claims 1
- -1 peptide Proteins 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 108020001580 protein domains Proteins 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
Claims (40)
X2は、Q又はEであり;
X3は、Y又はK(PEG4palm)であり;
X4は、E、R、K又はK(PEG4palm)であり;
X5は、Y又はK(PEG4palm)であり;
X6は、L又はK(PEG4palm)であり;
X7は、D又はEであり;
X8は、S、E又はK(PEG4palm)であり;
X9は、R、E、S、K(gEpalm)、K(PEG2palm)、K(PEG3palm)、K(PEG4palm)又はK(PEG2−PEG2−gEpalm)であり;
X10は、R、A、又はK(gEpalm)、K(PEG4palm)であり;
X11は、Q、R、A、E又はK(gEpalm)、K(PEG4palm)であり;
X12は、D又はK(gEpalm)であり;
X13は、Q、A又はEであり;
X14は、L又はEであり;
X15は、V又はEであり;
X16は、非存在であるか、又はAであり;
分子あたり1以下のリシンが、パルミトイル化される)
を含む単離ペプチド。 Amino acid sequence:
X 2 is Q or E;
X 3 is Y or K (PEG4 palm) ;
X 4 is E, R, K or K (PEG4palm);
X 5 is Y or K (PEG4 palm);
X 6 is L or K (PEG4 palm);
X 7 is D or E;
X 8 is S, E or K (PEG4 palm);
X 9 is R, E, S, K (gEpalm), K (PEG2palm), K (PEG3palm), K (PEG4palm), or K (PEG2-PEG2-gEpalm);
X 10 is R, A, or K (gEpalm), K (PEG4palm);
X 11 is Q, R, A, E or K (gEpalm), K (PEG4palm);
X 12 is D or K (gEpalm);
X 13 is Q, A or E;
X 14 is L or E;
X 15 is V or E;
X 16 is absent or is A;
Less than one lysine per molecule is palmitoylated)
An isolated peptide comprising
(a)
10、13、14、16、17、18、20又は21位のアミノ酸が、パルミトイル化リシンであるとき、12位のリシンは、パルミトイル化されず;
10、13、14、16、17、18、20及び21位のアミノ酸が、パルミトイル化リシンではないとき、12位のリシンは、任意選択でパルミトイル化され;また
前記ペプチドは、C末端アミノ酸で、(PEG)x2基によりペグ化されており、
ここで、x2は、2〜12である)
からなる群から選択されるアミノ酸配列
を含む、請求項1に記載の単離ペプチド。 The peptide is:
(A)
When the amino acid at position 10, 13, 14, 16, 17, 18, 20, or 21 is palmitoylated lysine, the lysine at position 12 is not palmitoylated;
When the amino acids at positions 10, 13, 14, 16, 17, 18, 20, and 21 are not palmitoylated lysine, the lysine at position 12 is optionally palmitoylated; and the peptide is the C-terminal amino acid, PEGylated by (PEG) x 2 groups,
Here, x 2 is a 2 to 12)
The isolated peptide of claim 1 comprising an amino acid sequence selected from the group consisting of.
Bは、K(gE−palm)であり;
B1は、K(PEG4−palm)であり;
B2は、K(PEG3−palm)であり;
B3は、K(PEG2−palm)であり;
B4は、K(PEG4−gE−palm)であり;
B5は、K(PEG2−gE−palm)であり;
B6は、K(PEG2−PEG2−gE−palm)である)
のアミノ酸配列を含む、請求項1に記載の単離ペプチド。 The peptide is:
B is K (gE-palm);
B 1 is K (PEG4-palm);
B 2 is K (PEG3-palm);
B 3 is K (PEG2-palm);
B 4 is K (PEG4-gE-palm);
B 5 is an K (PEG2-gE-palm) ;
B 6 is K (PEG2-PEG2-gE-palm))
The isolated peptide of claim 1 comprising the amino acid sequence of
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361783675P | 2013-03-14 | 2013-03-14 | |
US61/783,675 | 2013-03-14 | ||
PCT/EP2014/055034 WO2014140222A1 (en) | 2013-03-14 | 2014-03-13 | Pegylated glucagon and glp-1 co-agonists for the treatment of obesity |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2016512213A JP2016512213A (en) | 2016-04-25 |
JP2016512213A5 true JP2016512213A5 (en) | 2017-04-13 |
Family
ID=50272654
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015562166A Pending JP2016512213A (en) | 2013-03-14 | 2014-03-13 | Pegylated glucagon and GLP-1 co-agonist for the treatment of obesity |
Country Status (7)
Country | Link |
---|---|
US (1) | US9714277B2 (en) |
EP (2) | EP3238734A1 (en) |
JP (1) | JP2016512213A (en) |
AU (1) | AU2014230472A1 (en) |
CA (1) | CA2902352A1 (en) |
HK (1) | HK1220383A1 (en) |
WO (1) | WO2014140222A1 (en) |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6995042B2 (en) | 2016-05-24 | 2022-02-04 | 武田薬品工業株式会社 | Peptide compound |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UA116217C2 (en) | 2012-10-09 | 2018-02-26 | Санофі | Exendin-4 derivatives as dual glp1/glucagon agonists |
AR094180A1 (en) | 2012-12-21 | 2015-07-15 | Sanofi Sa | DERIVATIVES OF EXENDINA-4 |
AU2014272500B2 (en) | 2013-05-28 | 2018-03-08 | Scohia Pharma, Inc. | Peptide compound |
WO2015067716A1 (en) * | 2013-11-06 | 2015-05-14 | Zealand Pharma A/S | Glucagon-glp-1-gip triple agonist compounds |
EP3080152A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Non-acylated exendin-4 peptide analogues |
EP3080149A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Dual glp-1/glucagon receptor agonists |
WO2015086729A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/gip receptor agonists |
EP3080150B1 (en) | 2013-12-13 | 2018-08-01 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
TW201625670A (en) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | Dual GLP-1/glucagon receptor agonists derived from EXENDIN-4 |
TW201625668A (en) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | Exendin-4 derivatives as peptidic dual GLP-1/glucagon receptor agonists |
TW201625669A (en) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | Peptidic dual GLP-1/glucagon receptor agonists derived from Exendin-4 |
US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
AR105319A1 (en) | 2015-06-05 | 2017-09-27 | Sanofi Sa | PROPHARMS THAT INCLUDE A DUAL AGONIST GLU-1 / GLUCAGON CONJUGATE HIALURONIC ACID CONNECTOR |
TWI726889B (en) * | 2015-06-10 | 2021-05-11 | 英商梅迪繆思有限公司 | Protease-resistant lipidated peptides |
WO2016198628A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Non-acylated exendin-4 derivatives as dual glp-1/glucagon receptor agonists |
WO2016198624A1 (en) | 2015-06-12 | 2016-12-15 | Sanofi | Exendin-4 derivatives as trigonal glp-1/glucagon/gip receptor agonists |
AR105284A1 (en) | 2015-07-10 | 2017-09-20 | Sanofi Sa | DERIVATIVES OF EXENDINA-4 AS SPECIFIC DUAL PEPTIDE AGONISTS OF GLP-1 / GLUCAGÓN RECEPTORS |
RU2670983C1 (en) * | 2017-10-11 | 2018-10-29 | Федеральное государственное бюджетное учреждение "Государственный научно-исследовательский институт генетики и селекции промышленных микроорганизмов Национального исследовательского центра "Курчатовский институт" (НИЦ "Курчатовский институт" - ГосНИИгенетика) | Using a polypeptide derived from human glucagon-like peptide 1 as a means to control body weight |
TWI770085B (en) * | 2017-11-21 | 2022-07-11 | 日商武田藥品工業股份有限公司 | Peptide compound |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
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EP0154316B1 (en) | 1984-03-06 | 1989-09-13 | Takeda Chemical Industries, Ltd. | Chemically modified lymphokine and production thereof |
ATE135370T1 (en) | 1988-12-22 | 1996-03-15 | Kirin Amgen Inc | CHEMICALLY MODIFIED GRANULOCYTE COLONY EXCITING FACTOR |
US6440175B1 (en) | 2001-06-28 | 2002-08-27 | Stanley, Iii Virgil E. | Hair coloring kit |
AU2003273300A1 (en) * | 2002-09-06 | 2004-03-29 | Bayer Pharmaceuticals Corporation | Modified glp-1 receptor agonists and their pharmacological methods of use |
US20090202497A1 (en) * | 2005-08-23 | 2009-08-13 | The General Hospital Corporation | Use of glp-1, glp-1 derivatives or glp-1 fragments for skin regeneration, stimulation of hair growth, or treatment of diabetes |
PL2173890T3 (en) | 2007-06-21 | 2011-07-29 | Univ Muenchen Tech | Biological active proteins having increased in vivo and/or vitro stability |
PE20100255A1 (en) * | 2008-06-17 | 2010-04-25 | Univ Indiana Res & Tech Corp | GLUCAGON / GLP-1 RECEPTOR CO-AGONISTS |
IN2012DN00377A (en) * | 2009-06-16 | 2015-08-21 | Univ Indiana Res & Tech Corp | |
US9156901B2 (en) * | 2009-07-13 | 2015-10-13 | Ditte Riber | Acylated glucagon analogues |
ES2661228T3 (en) * | 2010-05-13 | 2018-03-28 | Indiana University Research And Technology Corporation | Glucagon superfamily peptides that show nuclear hormone receptor activity |
WO2012054822A1 (en) * | 2010-10-22 | 2012-04-26 | Nektar Therapeutics | Pharmacologically active polymer-glp-1 conjugates |
WO2012088116A2 (en) * | 2010-12-22 | 2012-06-28 | Indiana University Research And Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
WO2012150503A2 (en) * | 2011-05-03 | 2012-11-08 | Zealand Pharma A/S | Glu-glp-1 dual agonist signaling-selective compounds |
BR112013032717A2 (en) * | 2011-06-22 | 2017-01-24 | Univ Indiana Res & Tech Corp | glucagon / glp-1 receptor coagonists |
TWI674270B (en) * | 2012-12-11 | 2019-10-11 | 英商梅迪繆思有限公司 | Glucagon and glp-1 co-agonists for the treatment of obesity |
-
2014
- 2014-03-13 AU AU2014230472A patent/AU2014230472A1/en not_active Abandoned
- 2014-03-13 US US14/775,074 patent/US9714277B2/en not_active Expired - Fee Related
- 2014-03-13 JP JP2015562166A patent/JP2016512213A/en active Pending
- 2014-03-13 EP EP17174372.7A patent/EP3238734A1/en not_active Withdrawn
- 2014-03-13 CA CA2902352A patent/CA2902352A1/en not_active Abandoned
- 2014-03-13 WO PCT/EP2014/055034 patent/WO2014140222A1/en active Application Filing
- 2014-03-13 EP EP14709713.3A patent/EP2968581A1/en not_active Withdrawn
-
2016
- 2016-07-19 HK HK16108513.3A patent/HK1220383A1/en unknown
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP6995042B2 (en) | 2016-05-24 | 2022-02-04 | 武田薬品工業株式会社 | Peptide compound |
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